DE60300502D1 - Process for the preparation of citalopram - Google Patents

Process for the preparation of citalopram

Info

Publication number
DE60300502D1
DE60300502D1 DE60300502T DE60300502T DE60300502D1 DE 60300502 D1 DE60300502 D1 DE 60300502D1 DE 60300502 T DE60300502 T DE 60300502T DE 60300502 T DE60300502 T DE 60300502T DE 60300502 D1 DE60300502 D1 DE 60300502D1
Authority
DE
Germany
Prior art keywords
citalopram
preparation
cyanophthalide
cyclized
bromine
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
DE60300502T
Other languages
German (de)
Other versions
DE60300502T2 (en
Inventor
Giovanni Cotticelli
Lernia Gianluca Di
Milanesi Silvia
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Adorkem Technology SpA
Original Assignee
Adorkem Technology SpA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Adorkem Technology SpA filed Critical Adorkem Technology SpA
Application granted granted Critical
Publication of DE60300502D1 publication Critical patent/DE60300502D1/en
Publication of DE60300502T2 publication Critical patent/DE60300502T2/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F3/00—Compounds containing elements of Groups 2 or 12 of the Periodic Table
    • C07F3/003—Compounds containing elements of Groups 2 or 12 of the Periodic Table without C-Metal linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Steroid Compounds (AREA)

Abstract

A method for the preparation of citalopram and its pharmaceutically acceptable salts is described; it's obtained starting from 5-cyanophthalide by reaction with a mixture of 4-fluorophenyl magnesium bromide and 3-dimethylaminopropyl magnesium chloride. The intermediate obtained is showed here-below: <CHEM> wherein X is an halogen, preferably chlorine or bromine, which is cyclized without any isolation.
DE60300502T 2003-10-28 2003-10-28 Process for the preparation of citalopram Expired - Fee Related DE60300502T2 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03425693A EP1506963B1 (en) 2003-10-28 2003-10-28 Method for the preparation of citalopram

Publications (2)

Publication Number Publication Date
DE60300502D1 true DE60300502D1 (en) 2005-05-19
DE60300502T2 DE60300502T2 (en) 2006-02-23

Family

ID=33560918

Family Applications (2)

Application Number Title Priority Date Filing Date
DE60300502T Expired - Fee Related DE60300502T2 (en) 2003-10-28 2003-10-28 Process for the preparation of citalopram
DE602004019127T Expired - Fee Related DE602004019127D1 (en) 2003-10-28 2004-10-22 PROCESS FOR THE PREPARATION OF CITALOPRAM

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE602004019127T Expired - Fee Related DE602004019127D1 (en) 2003-10-28 2004-10-22 PROCESS FOR THE PREPARATION OF CITALOPRAM

Country Status (15)

Country Link
US (1) US20070060759A1 (en)
EP (2) EP1506963B1 (en)
JP (1) JP2007511477A (en)
CN (1) CN1875013A (en)
AT (2) ATE293106T1 (en)
BR (1) BRPI0415778A (en)
CA (1) CA2543155A1 (en)
DE (2) DE60300502T2 (en)
DK (2) DK1506963T3 (en)
ES (1) ES2240931T3 (en)
HK (1) HK1075041A1 (en)
PL (1) PL379659A1 (en)
PT (1) PT1506963E (en)
SI (1) SI1506963T1 (en)
WO (1) WO2005049595A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8470885B2 (en) 2009-01-12 2013-06-25 Biokier, Inc. Composition and method for treatment of diabetes
US9314444B2 (en) 2009-01-12 2016-04-19 Biokier, Inc. Composition and method for treatment of NASH
US9006288B2 (en) 2009-01-12 2015-04-14 Biokier, Inc. Composition and method for treatment of diabetes
US9301938B2 (en) 2009-09-23 2016-04-05 Biokier, Inc. Composition and method for treatment of diabetes
BR112013028104A2 (en) 2011-05-02 2020-08-04 Biokier, Inc. composition and method for treating diabetes
US20150073057A1 (en) 2013-09-06 2015-03-12 Biokier, Inc. Composition and method for treatment of diabetes
CN111302971B (en) * 2018-12-12 2023-08-22 上海奥博生物医药股份有限公司 Method for continuously preparing 5-cyanodiol

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1526331A (en) * 1976-01-14 1978-09-27 Kefalas As Phthalanes
GB8419963D0 (en) * 1984-08-06 1984-09-12 Lundbeck & Co As H Intermediate compound and method
GB8814057D0 (en) * 1988-06-14 1988-07-20 Lundbeck & Co As H New enantiomers & their isolation
EP1015416B1 (en) * 1997-07-08 2001-09-19 H. Lundbeck A/S Method for the preparation of citalopram
UA62985C2 (en) * 1997-11-10 2004-01-15 Lunnbeck As H A method for the preparation of citalopram
CZ292911B6 (en) * 1997-11-11 2004-01-14 H. Lundbeck A/S Process for preparing citalopram
EP1355897A1 (en) * 2001-01-30 2003-10-29 Orion Corporation Fermion Process for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile
US6967259B2 (en) * 2001-09-24 2005-11-22 Pharmachem Technologies Limited Process for the preparation of Citalopram intermediate

Also Published As

Publication number Publication date
ES2240931T3 (en) 2005-10-16
US20070060759A1 (en) 2007-03-15
ATE420870T1 (en) 2009-01-15
DE602004019127D1 (en) 2009-03-05
EP1506963A1 (en) 2005-02-16
ATE293106T1 (en) 2005-04-15
DE60300502T2 (en) 2006-02-23
EP1682526B1 (en) 2009-01-14
SI1506963T1 (en) 2005-10-31
DK1506963T3 (en) 2005-08-01
CN1875013A (en) 2006-12-06
JP2007511477A (en) 2007-05-10
PL379659A1 (en) 2006-10-30
BRPI0415778A (en) 2006-12-26
CA2543155A1 (en) 2005-06-02
WO2005049595A1 (en) 2005-06-02
EP1682526A1 (en) 2006-07-26
EP1506963B1 (en) 2005-04-13
HK1075041A1 (en) 2005-12-02
DK1682526T3 (en) 2009-03-23
PT1506963E (en) 2005-08-31

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee